YANG Lu, SHI Hang, LI Yun-lan, CHEN Xi, NIU Si-qing, QIAO Xiao-zhi, MAI Jia-qi, LI Qing-shan. Synthesis and anti-inflammatory activity of novel isobutyl benzophenone derivativesJ. Acta Pharmaceutica Sinica, 2018,53(2): 256-262. doi: 10.16438/j.0513-4870.2017-1224
Citation: YANG Lu, SHI Hang, LI Yun-lan, CHEN Xi, NIU Si-qing, QIAO Xiao-zhi, MAI Jia-qi, LI Qing-shan. Synthesis and anti-inflammatory activity of novel isobutyl benzophenone derivativesJ. Acta Pharmaceutica Sinica, 2018,53(2): 256-262. doi: 10.16438/j.0513-4870.2017-1224

Synthesis and anti-inflammatory activity of novel isobutyl benzophenone derivatives

  • Twenty target compounds were synthesized by the reduction reaction of HUANG Minglong and Friedel-Crafts acylation reaction in this study. The inhibitory effects of the new compounds were tested on NO production in LPS-induced mouse macrophage RAW264.7 cells, a cellular inflammation model. The structure-activity relationships were discussed. The structures of target compounds were confirmed by ESI-MS, 1H NMR and 13C NMR. In vitro activity experiments showed that 18 compounds had certain anti-inflammatory effects at the concentration of 40 μmol·L-1, of which 9a, 8b, 7c and 9c showed strong anti-inflammatory activities, and IC50 of 7c and 9c were comparable to the positive control drug ibuprofen.
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